ACY-738

Catalog No.S8648

For research use only.

ACY-738 inhibits HDAC6 with low nanomolar potency (IC50=1.7 nM) and a selectivity of 60- to 1500-fold over class I HDACs.

ACY-738 Chemical Structure

CAS No. 1375465-91-0

Selleck's ACY-738 has been cited by 2 Publications

Purity & Quality Control

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Biological Activity

Description ACY-738 inhibits HDAC6 with low nanomolar potency (IC50=1.7 nM) and a selectivity of 60- to 1500-fold over class I HDACs.
Targets
HDAC6 [1]
(Cell-free)
1.7 nM
Assay
Methods Test Index PMID
Western blot acet α-tubulin 27957719
Immunofluorescence acet H3 / acet α-tubulin 27957719
In vivo ACY-738 induces dramatic increases in α-tubulin acetylation in brain and stimulate mouse exploratory behaviors in novel, but not familiar environments. ACY-738 has the antidepressant-like properties. Elimination of ACY-738 from plasma is rapid, with plasmatic half-life of 12 min and concentration below 10 ng/ml after 2 h. ACY-738 rapidly distributes to the brain leading to a total drug exposure in CNS comparable to that of peripheral tissues[1]. ACY-738 decreases several characteristics of SLE (Systemic lupus erythematosus) in NZB/W mice by dictating B cell development in the bone marrow. ACY-738 treatment increases the percentage of B cells in early developmental stages, while decreasing the percentage of cells in late pre-B cell fraction F. ACY-738 regulation of BM B cell development could be due to regulation developmental checkpoints known to be dysfunctional during SLE[2].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: Undifferentiated RN46A-B14 cells
  • Concentrations: 2.5 μM
  • Incubation Time: 4 h
  • Method:

    Undifferentiated RN46A-B14 cells, a line of immortalized rat raphe neuronal precursors, are grown. They are treated with 2.5 μM ACY-738, ACY-775, tubastatin A, or 0.6 μM TSA, or vehicle (0.1% DMSO) for 4 h. Samples are processed using Epigentek histone extraction kit and quantified using protein assay.

  • (Only for Reference)
Animal Research:

[1]

  • Animal Models: Male NIH Swiss mice
  • Dosages: 5 mg/kg
  • Administration: i.p.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 54 mg/mL
(199.78 mM)
Ethanol 1 mg/mL
(3.69 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 270.29
Formula

C14H14N4O2

CAS No. 1375465-91-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC1(C2=CC=CC=C2)NC3=NC=C(C=N3)C(=O)NO

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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